Medchemexpress/Daclatasvir(Synonyms: BMS-790052; EBP 883)/HY-10466/5mg_蚂蚁淘，【正品极速】生物医学科研用品轻松购|ebiomall 蚂蚁淘商城

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Medchemexpress/Daclatasvir(Synonyms: BMS-790052; EBP 883)/HY-10466/5mg

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Medchemexpress/Daclatasvir(Synonyms: BMS-790052; EBP 883)/HY-10466/5mg

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MedChemExp

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HY-10466-10mM*1mLinDMSO

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4000-520-616

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DaclatasvirisapotentHCVNS5Aproteininhibitor,withmeanEC₅₀valuesof50and9pMagainstgenotype1aand1breplicons,respectively.

CustomerValidation

•EMBORep.2016Jul;17(7):1013-28.
•PLoSPathog.2017May11;13(5):e1006374.
•IntJRADIatOncolBiolPhys.2016Nov15;96(4):867-876.
•JVirol.2014May;88(10):5578-94.
•FrontPharmacol.2016Dec21;7:490.
•IntJAntimicrobAgents.2015Oct;46(4):381-8.

•AntimicrobAgentsChemother.2015May;59(5):2496-507.
•AntimicrobAgentsChemother.2014Aug;58(8):4555-64.
•AntimicrobAgentsChemother.2014Jun;58(6):3327-34.
•AntimicrobAgentsChemother.2013Mar;57(3):1180-91.
•AntiviralRes.2017Oct;146:191-200.
•AntiviralRes.2017Oct23;148:5-14.
•PLoSOne.2016Jul21;11(7):e0159511.
•PLoSOne.2016Apr22;11(4):e0152036.
•PLoSOne.2015Aug11;10(8):e0134707.
•VirusRes.2017Mar18;235:37-48.
•TransplInfectDis.2017Nov7.
•HepatolCommun.2017;1(6).
•HepatolCommun.June6,2017.
•OpenVirolJ.2014Mar7;8:1-8.

Description

DaclatasvirisapotentHCVNS5Aproteininhibitor,withmeanEC₅₀valuesof50and9pMagainstgenotype1aand1breplicons,respectively.

IC₅₀&Target

EC50:9±4pM(HCVreplicongenotype1b,inCon1cells),50±13pM(HCVreplicongenotype1a,inH77cells)^[1]

InVitro

Daclatasvir(BMS-790052)isasmallmoleculeinhibitoroftheHCVNS5Aproteinthatexhibitspicomolarhalf-maximumeffectiveconcentrations(EC₅₀)towardsrepliconsexpressingabroadrangeofHCVgenotypesandtheJFH-1genotype2ainfectiousvirusincellculture.DaclatasvirisapotentinhibitoroftheJFH-1genotype2ainfectiousvirusthatreplicatesincellculture(EC₅₀=28pM),anassayconsideredtobeamoreBIOLOGicallyrelevantinvitrocellculturesystem.Inaddition,DaclatasvirdisplayssimilarpotencyinHuh-7,HeLaandHEK293Tcells,demonstratingthatthefunction(s)ofNS5AinhibitedbyDaclatasviris(are)highlyconservedindifferentcellularenvironments^[1].

InVivo

Inarandomized,double-blind,placebo-controlled,singleascending-dosestudy,Daclatasvir(BMS-790052)isadmiNISTeredatsixdoselevelstohealthy,non-HCV-infectedsubjectsoverarangeof1to200mgasanoralsolution.Daclatasvirissafeandwelltoleratedupto200mgwithnoclinicallyrelevantadverseeffects.Afteroraladministration,Daclatasvirisreadilyabsorbed,withdose-proportionalexposuresoverthestudieddoserange,andallsubjectshavedrugconcentrationsgreaterthantheprotein-binding-adjustedEC₉₀forgenotypes1aand1b,asmeasuredintherepliconassay,atandbeyond24hpost-dose.(Theproteinbinding-adjustedEC₉₀figuresarederivedfromananalysisoftheeffectoftheadditionofhumanserumonantiviralactivityinreplicons.Inthepresenceof40%humanserum,theEC₉₀forDaclatasviris383pM(0.28ng/mL)forthegenotype1arepliconand49pM(0.04ng/mL)forthegenotyope1breplicon)^[1].MiceineachgroupthatdevelopedpersistentHCVinfectionaredividedintotwotreatmentgroups.Onegroupreceive4weeksofAsunaprevir/Daclatasvirtreatmentandtheothergroupreceived4weeksofLedipasvir/GS-558093treatment.Asunaprevir/DaclatasvirtherapyandLedipasvir/GS-558093therapyrapidlydeceaseserumHCVRNAlevelstobelowthesensitivity,andtheyarenotdetectedaftercompletionofthetherapyexceptfortwomiceintheLedipasvir/GS-558093group^[2].

ClinicalTrial

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References

[1].GaoM,etal.ChemicalgeneticsstrategyidentifiesanHCVNS5Ainhibitorwithapotentclinicaleffect.Nature.2010May6;465(7294):96-100.
[2].KaiY,etal.EmergenceofhepatitisCvirusNS5AL31VplusY93HvariantupontreatmentfailureofdaclatasvirandasunaprevirisrelativelyresistanttoledipasvirandNS5BpolymerasenucleotideinhibitorGS-558093inhumanhepatocytechimericmice.JGa

PreparingStockSolutions

ConcentrationVolumeMass	1mg	5mg	10mg

1mM	1.3534mL	6.7670mL	13.5340mL
5mM	0.2707mL	1.3534mL	2.7068mL
10mM	0.1353mL	0.6767mL	1.3534mL

Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.

CellAssay
^[1]

Daclatasvir(BMS-790052)isdissolvedinDMSOandstored,andthendilutedwithappropriatemediabeforeuse^[1].

HCVgenotype1aand1brepliconcellsaremaintainedinmediacontainingDaclatasvirataconcentrationof5-to20-foldaboveEC₅₀and0.5mg/mLG418.RepliconcellssimilarlytreatedwithDMSOaremaintainedascontrols.Afterapproximately4-5weekswhencellgrowthissimilartoDMSO-treatedcontrolcells,selectedcellsareexpandedforresistancetestingandanalysisbyPCRwithreversetranscription^[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
^[2]

Daclatasvir(BMS-790052)isdissolvedinDMSOanddilutedwithsaline^[2].

Mice^[2]
Humanizedliverchimericmice,whosechimericrateoftheliverisestimatedasover40%,areinjectedintravenouslywith100µLofHCV-positivehumanserumsamples.Afterinoculation,theirbloodiscollectedfromanexternaljugularveinevery1-4weeks.TheHCVRNAlevelsaremeasuredbytheCOBASTaqManHCVtestin100-folddilutedserumwithalowermeasurementrangeof3.2logIU/mLserum.AfterserumlevelsofHCVRNAreachplateaulevels,miceareadministeredorallyonceadayfor4weekswithoneofthefollowing:40mg/kgofAsunaprevirplus30mg/kgofDaclatasvir,15mg/kgofLedipasvirplus50mg/kgofGS-558093and50mg/kgofGS-558093plus400mg/kgofTelaprevir.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

[1].GaoM,etal.ChemicalgeneticsstrategyidentifiesanHCVNS5Ainhibitorwithapotentclinicaleffect.Nature.2010May6;465(7294):96-100.
[2].KaiY,etal.EmergenceofhepatitisCvirusNS5AL31VplusY93HvariantupontreatmentfailureofdaclatasvirandasunaprevirisrelativelyresistanttoledipasvirandNS5BpolymerasenucleotideinhibitorGS-558093inhumanhepatocytechimericmice.JGa

MolecularWeight

738.88

Formula

C₄₀H₅₀N₈O₆

CASNo.

1009119-64-5

Storage

Powder	-20°C	3years
	4°C	2years
Insolvent	-80°C	6months
	-20°C	1month

Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥40mg/mL

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:99.31%

SelectBatch: